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41. 发明申请

WO2003032962A2 DUAL ACTION ANTIBIOTICS 审中-公开
标题翻译：双作用抗生素
公开(公告)号：WO2003032962A2
公开(公告)日：2003-04-24
申请号：PCT/EP2002/011163
申请日：2002-10-04
申请人： MORPHOCHEM AKTIENGESELLSCHAFT FÜR KOMBINATORISCHE CHEMIE , HUBSCHWERLEN, Christian , SPECKLIN, Jean-Luc
发明人： HUBSCHWERLEN, Christian , SPECKLIN, Jean-Luc
IPC分类号： A61K31/00
CPC分类号： C07D413/12 , C07D413/14 , C07D471/04
摘要： The present invention relates to compounds of the Formula (I) that are useful antimicrobial agents and effective against a variety of multi-drug resistant bacteria.
摘要翻译：本发明涉及作为有用的抗微生物剂的式I化合物，并且能有效地抵抗多种耐药性细菌。

42. 发明申请

WO2003031443A1 DUAL ACTIONS ANTIBIOTICS COMPRISING A OXAZOLDINONE AND A QUINOLONE OR NAPHTHYRIDINONE MOIETY 审中-公开
标题翻译：包含奥沙喹酮和喹啉酮或萘啶酮酮的双作用抗生素
公开(公告)号：WO2003031443A1
公开(公告)日：2003-04-17
申请号：PCT/EP2002/010766
申请日：2002-09-25
申请人： MORPHOCHEM AKTIENGESELLSCHAFT FÜR KOMBINATORISCHE CHEMIE , HUBSCHWERLEN, Christian , SPECKLIN, Jean-Luc
发明人： HUBSCHWERLEN, Christian , SPECKLIN, Jean-Luc
IPC分类号： C07D413/14
CPC分类号： C07D413/12 , C07D413/14 , C07D471/04
摘要： The present invention relates to compounds of the Formula (I) that are useful antimicrobial agents and effective against a variety of multi-drug resistant bacteria.
摘要翻译：本发明涉及作为有用的抗微生物剂并能有效抵抗各种多重耐药性细菌的式（I）化合物。

43. 发明申请

WO2013038374A1 PROCESS FOR MANUFACTURING A SYNTHETIC INTERMEDIATE 审中-公开
标题翻译：制造合成中间体的方法
公开(公告)号：WO2013038374A1
公开(公告)日：2013-03-21
申请号：PCT/IB2012/054804
申请日：2012-09-14
申请人： ACTELION PHARMACEUTICALS LTD , ABELE, Stefan , BERGNER, Eike, J. , BUKOVEC, Christian , FUNEL, Jacques-Alexis , HUBSCHWERLEN, Christian , MIRRE, Azely , SCHINDELHOLZ, Ivan , SURIVET, Jean-Philippe , ZUMBRUNN ACKLIN, Cornelia
发明人： ABELE, Stefan , BERGNER, Eike, J. , BUKOVEC, Christian , FUNEL, Jacques-Alexis , HUBSCHWERLEN, Christian , MIRRE, Azely , SCHINDELHOLZ, Ivan , SURIVET, Jean-Philippe , ZUMBRUNN ACKLIN, Cornelia
IPC分类号： C07D497/04
CPC分类号： C07D497/04
摘要： The invention relates to a process for manufacturing the compound of formula 1-6 which is a synthetic intermediate commonly used in the preparation of antibiotic compounds, or for manufacturing salts of that compound. The invention furthermore relates to intermediate compounds used in such process, namely 6,7-dihydro- [l,4]oxathiino[2,3-c]pyridazin-3(2H)-one, 6,7-dihydro-[l,4]oxathiino[2,3-c]pyridazin-3-yl trifluoromethanesulfonate and methyl 6,7-dihydro-[l,4]oxathiino[2,3-c]pyridazine- 3-carboxylate, and to salts thereof.
摘要翻译：本发明涉及一种制备式1-6化合物的方法，其为通常用于制备抗生素化合物的合成中间体，或用于制备该化合物的盐。本发明还涉及用于该方法的中间体化合物，即6,7-二氢 - [1,4]氧硫杂环[2,3-c]哒嗪-3（2H） - 酮，6,7-二氢 - 4]氧硫杂环[2,3-c]哒嗪-3-基三氟甲磺酸酯和6,7-二氢 - [1,4]氧硫杂环[2,3-c]哒嗪-3-羧酸甲酯及其盐。

44. 发明申请

WO2013021363A1 QUINAZOLINE-2,4-DIONE DERIVATIVES 审中-公开
标题翻译：喹唑啉-2,4-二酮衍生物
公开(公告)号：WO2013021363A1
公开(公告)日：2013-02-14
申请号：PCT/IB2012/054080
申请日：2012-08-10
申请人： ACTELION PHARMACEUTICALS LTD , HUBSCHWERLEN, Christian , SURIVET, Jean-Philippe , RUEEDI, Georg , ZUMBRUNN ACKLIN, Cornelia
发明人： HUBSCHWERLEN, Christian , SURIVET, Jean-Philippe , RUEEDI, Georg , ZUMBRUNN ACKLIN, Cornelia
IPC分类号： C07D413/14 , C07D417/14 , C07D498/04 , C07D513/04 , A61K31/538 , A61K31/5383 , A61K31/5415 , A61K31/542 , A61P31/04 , A61P31/06 , A61P33/02
CPC分类号： C07D471/04 , C07D413/14 , C07D417/14 , C07D498/04 , C07D513/04
摘要： The invention relates to antibacterial compounds of formula (I), wherein R 1 is H, halogen, (C 1 -C 3 )alkyl or (C 1 -C 3 )alkoxy; R 2 is H, halogen, (C 1 -C 3 )alkyl, (C 1 -C 3 )alkoxy or pyrrolidin-l-yl; R 3 is H, halogen, (C 1 -C 3 )alkyl, (C 1 -C 3 )alkoxy, vinyl or 2-methoxycarbonylvinyl or R 2 and R 3 together with the two carbon atoms which bear them form a phenyl ring; R 4 is H, halogen, (C 1 -C 3 )alkyl or (C 1 -C 3 )alkoxy and R5 is H, (C1-C3)alkyl or cyclopropyl, or R 4 and R 5 form together a -CH 2 CH 2 CH 2 - group; A is the divalent group -CH 2 -, -CH 2 CH 2 -, #-CH(OH)CH 2 -*, #-CH 2 N(R 6 )-* or -CH 2 NHCH 2 -, wherein # indicates the point of attachment to the optionally substituted (quinazoline-2,4-dione-3-yl)methyl residue and * represents the point of attachment to the substituted (oxazolidinon-4-yl)methyl residue; R 6 is H or acetyl; Y is CH or N; and Q is O or S; and salts of such compounds.
摘要翻译：本发明涉及式（I）的抗菌化合物，其中R1是H，卤素，（C1-C3）烷基或（C1-C3）烷氧基; R2是H，卤素，（C1-C3）烷基，（C1-C3）烷氧基或吡咯烷-1-基; R3是H，卤素，（C1-C3）烷基，（C1-C3）烷氧基，乙烯基或2-甲氧基羰基乙烯基或R2和R3与它们携带的两个碳原子形成苯环; R4是H，卤素，（C1-C3）烷基或（C1-C3）烷氧基，R5是H，（C1-C3）烷基或环丙基，或R4和R5一起形成-CH2CH2CH2-基团; A是二价基团-CH 2 - ， - CH 2 CH 2 - ， - CH 2 OH，CH 2 - ， - CH 2 OH（R 6） - 或-CH 2 NHCH 2 - ，其中＃表示与任选取代的（喹唑啉 - 2,4-二酮-3-基）甲基残基，*表示与取代的（恶唑烷酮-4-基）甲基残基的连接点; R6是H或乙酰基; Y是CH或N; Q为O或S; 和这些化合物的盐。

45. 发明申请

WO2009104159A1 OXAZOLIDINONE DERIVATIVES 审中-公开
标题翻译：氧杂环丁酮衍生物
公开(公告)号：WO2009104159A1
公开(公告)日：2009-08-27
申请号：PCT/IB2009/050702
申请日：2009-02-20
申请人： ACTELION PHARMACEUTICALS LTD , HUBSCHWERLEN, Christian , RUEEDI, Georg , SURIVET, Jean-Philippe , ZUMBRUNN ACKLIN, Cornelia
发明人： HUBSCHWERLEN, Christian , RUEEDI, Georg , SURIVET, Jean-Philippe , ZUMBRUNN ACKLIN, Cornelia
IPC分类号： C07D413/14 , C07D417/14 , C07D417/04 , C07D519/00 , A61K31/536 , A61K31/4704 , A61K31/498 , A61K31/4985 , A61P31/00
CPC分类号： C07D417/14 , C07D413/14 , C07D471/04 , C07D519/00
摘要： The invention relates to compounds of Formula (I) wherein U, V, W, R 1 , R 1b , A and G are as defined in the description, to pharmaceutically acceptable salts of such compounds and to the use of these compounds in the manufacture of a medicament for the prevention or treatment of a bacterial infection.
摘要翻译：本发明涉及其中U，V，W，R 1，R 1b，A和G如说明书中所定义的式（I）化合物与这些化合物的药学上可接受的盐以及这些化合物在制备用于预防或治疗细菌感染的药物。

46. 发明申请

WO2009034546A2 TRANS-DECAHYDROISOQUINOLINE DERIVATIVES 审中-公开
标题翻译：十二氢异喹啉衍生物
公开(公告)号：WO2009034546A2
公开(公告)日：2009-03-19
申请号：PCT/IB2008053688
申请日：2008-09-12
申请人： ACTELION PHARMACEUTICALS LTD , HUBSCHWERLEN CHRISTIAN , RUEEDI GEORG , SURIVET JEAN-PHILIPPE , ZUMBRUNN ACKLIN CORNELIA
发明人： HUBSCHWERLEN CHRISTIAN , RUEEDI GEORG , SURIVET JEAN-PHILIPPE , ZUMBRUNN ACKLIN CORNELIA
CPC分类号： C07D401/04 , C07D471/04 , C07D498/04 , C07D513/04
摘要： The invention relates to antibacterial compounds of formula (I) wherein R1 is alkoxy, one or two of U, V, W, X represent(s) N, the remaining represents CH, whereby V may also represent CRa, W may also represent CRb and X may also represent CRC, Ra is hydroxyalkyl; Rb is alkoxycarbonyl, carboxy or hydroxyalkyl; Rc is halogen, R2is alkoxycarbonyl, carboxy, hydroxyalkyl or aminoalkyl, A is CH2B, C(=O)B or CH2CH=CHD, B is the group (II) wherein Z is N or CH and the ring P is selected from the formula (III) in which Q is O or S, and D is aryl (e.g. 1,4-difluoro-2 -phenyl).
摘要翻译：本发明涉及式（I）的抗菌化合物，其中R 1是烷氧基，U，V，W中的一个或两个表示（S）N，其余表示CH，其中V也可以表示CR a，W也可以表示CRb X也可以表示CRC，Ra是羟烷基; Rb是烷氧基羰基，羧基或羟烷基; R c是卤素，R 2是烷氧基羰基，羧基，羟基烷基或氨基烷基，A是CH 2 B，C（= O）B或CH 2 CH = CHD，B是其中Z是N或CH并且环P选自式（III）其中Q为O或S，D为芳基（如1,4-二氟-2-苯基）。

47. 发明申请

WO2008152603A1 3-AMINO-6-(1-AMINO-ETHYL)-TETRAHYDROPYRAN DERIVATIVES 审中-公开
标题翻译： 3-氨基-6-（1-氨基 - 乙基） - 羟基衍生物衍生物
公开(公告)号：WO2008152603A1
公开(公告)日：2008-12-18
申请号：PCT/IB2008/052333
申请日：2008-06-13
申请人： ACTELION PHARMACEUTICALS LTD , HUBSCHWERLEN, Christian , RUEEDI, Georg , SURIVET, Jean-Philippe , ZUMBRUNN ACKLIN, Cornelia
发明人： HUBSCHWERLEN, Christian , RUEEDI, Georg , SURIVET, Jean-Philippe , ZUMBRUNN ACKLIN, Cornelia
IPC分类号： C07D405/06 , C07D413/14 , C07D471/04 , C07D498/04 , C07D513/04 , C07D519/00 , A61K31/4375 , A61K31/4709 , A61P31/04
CPC分类号： C07D498/04 , C07D405/06 , C07D413/14 , C07D471/04 , C07D513/04 , C07D519/00
摘要： The invention relates to antibacterial compounds of formula I wherein R 1 represents halogen or alkoxy; U and W each represent N, V represents CH and R 2 represents H or F, or U and V each represent CH, W represents N and R 2 represents H or F, or U represents N, V represents CH, W represents CH or CR a and R 2 represents H, or also, when W represents CH, may represent F; R a represents CH 2 OH or alkoxycarbonyl; A represents the group CH=CH-B, a binuclear heterocyclic system D, a phenyl group which is mono substituted in position 4 by alkyl, or a phenyl group which is disubstituted in positions 3 and 4, wherein each of the substituents is independently selected from alkyl and halogen, B representing a mono- or di-substituted phenyl group wherein each substituent is a halogen atom and D representing the group wherein Z represents CH or N, and Q represents O or S; and to salts of such compounds.
摘要翻译：本发明涉及式I的抗菌化合物，其中R 1表示卤素或烷氧基; U和W各自表示N，V表示CH，R 2表示H或F，或U和V各自表示CH，W表示N，R 2表示H或F，或U表示N，V表示CH，W表示CH或CRa， R2表示H，或者当W表示CH时，可以表示F; Ra表示CH 2 OH或烷氧基羰基; A表示基团CH = CH-B，双核杂环体系D，在4位被烷基单取代的苯基或在3和4位被二取代的苯基，其中每个取代基被独立地选择由烷基和卤素组成，B代表一或二取代的苯基，其中每个取代基是卤素原子，D代表其中Z代表CH或N，Q代表O或S的基团; 和这些化合物的盐。

48. 发明申请

WO2008126034A3 OXAZOLIDINONE ANTIBIOTICS 审中-公开
公开(公告)号：WO2008126034A3
公开(公告)日：2008-10-23
申请号：PCT/IB2008/051374
申请日：2008-04-11
申请人： ACTELION PHARMACEUTICALS LTD , BUR, Daniel , HUBSCHWERLEN, Christian , RUEEDI, Georg , SURIVET, Jean-Philippe , ZUMBRUNN ACKLIN, Cornelia
发明人： BUR, Daniel , HUBSCHWERLEN, Christian , RUEEDI, Georg , SURIVET, Jean-Philippe , ZUMBRUNN ACKLIN, Cornelia
IPC分类号： C07D471/04 , A61K31/435 , A61P31/00 , C07D519/00
摘要： The invention relates to compounds of formula (I) wherein U, V, W, X, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , A, B, D, E, G, m and n are as defined in the description, to pharmaceutically acceptable salts of such compounds for use in the manufacture of a medicament for the prevention or treatment of a bacterial infection. Certain compounds of formula (I) are new and are also part of this invention.

49. 发明申请

WO2008126024A2 OXAZOLIDINONE ANTIBIOTIC DERIVATIVES 审中-公开
标题翻译：奥沙利汀抗生素衍生物
公开(公告)号：WO2008126024A2
公开(公告)日：2008-10-23
申请号：PCT/IB2008/051356
申请日：2008-04-10
申请人： ACTELION PHARMACEUTICALS LTD , GUDE, Markus , HUBSCHWERLEN, Christian , RUEEDI, Georg , SURIVET, Jean-Philippe , ZUMBRUNN ACKLIN, Cornelia
发明人： GUDE, Markus , HUBSCHWERLEN, Christian , RUEEDI, Georg , SURIVET, Jean-Philippe , ZUMBRUNN ACKLIN, Cornelia
IPC分类号： C07D471/04 , C07D413/14 , C07D417/14 , A61K31/4375 , A61P31/04
CPC分类号： C07D471/04 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： The invention relates to antibacterial compounds of formula (I) wherein R 1 is hydrogen, halogen, hydroxy, alkoxy or cyano; Y 1 and Y 2 each represent CH, one or two of U, V, W and X represent(s) N and the remaining each represent CH or, in the case of X, may also represent CR a , R a being halogen, and, in the case of W, may also represent CR b , or each of U, V, W, X, Y 1 and Y 2 represents CH, or each of U, V, W, X and Y 1 represents CH and Y 2 represents N, or also one or, provided R 1 is hydrogen, two of U, V, W, X, Y 1 and Y 2 represent(s) CRC and the remaining each represent CH, R b being alkoxy, alkoxycarbonyl or alkoxyalkoxy and R c being, each time it occurs, independently represents hydroxy or alkoxy; A-B-D represents a chain of 4 to 6 atoms, which 4 to 6 atoms are seleted from carbon, oxygen and nitrogen and may be substituted; E is one of the following groups: in which Z is CH or N and Q is O or S, or E is a phenyl group which is substituted once or twice in the meta and/or para position(s); and to salts of such compounds.
摘要翻译：本发明涉及其中R 1为氢，卤素，羟基，烷氧基或氰基的式（I）抗菌化合物; Y 1和Y 2各自表示CH，U，V，W和X中的一个或者两个表示（s）N，其余各自表示CH，或者在这种情况下的X，也可以表示CR a，R a，O，O是卤素，并且在W的情况下也可以表示CR b，或 U，V，W，X，Y 1和Y 2中的每一个表示CH，或U，V，W，X和Y 1中的每一个， SUP>表示CH，Y 2表示N，或者也可以是一个，或者如果R 1是氢，则U，V，W，X，Y 1中的两个＆lt; / 2＆gt;和＆lt; 2＆gt;代表CRC，其余各自表示CH，R b是烷氧基，烷氧基羰基或烷氧基烷氧基和R c 每次发生时，独立地表示羟基或烷氧基; A-B-D表示4至6个原子的链，其中4至6个原子从碳，氧和氮中分离并可以被取代; E是以下组之一：其中Z为CH或N且Q为O或S，或E为在间位和/或对位取代一次或两次的苯基; 和这些化合物的盐。

50. 发明申请

WO2007105154A3 ANTIBIOTIC COMPOUNDS 审中-公开
公开(公告)号：WO2007105154A3
公开(公告)日：2007-09-20
申请号：PCT/IB2007/050784
申请日：2007-03-09
申请人： ACTELION PHARMACEUTICALS LTD , GAUVIN, Jean-Christophe , HUBSCHWERLEN, Christian , SURIVET, Jean-Philippe , ZUMBRUNN ACKLIN, Cornelia
发明人： GAUVIN, Jean-Christophe , HUBSCHWERLEN, Christian , SURIVET, Jean-Philippe , ZUMBRUNN ACKLIN, Cornelia
IPC分类号： C07D405/06 , C07D409/14 , C07D471/04 , C07D495/04 , C07D519/00 , A61K31/519 , A61P31/04
摘要： The invention relates to selected antibiotics of formula (Al) wherein R 1 represents alkyl, alkoxy, haloalkoxy, halogen or cyano; one or two of U, V, W and X represent(s) N, the remaining represent CH, or, in case of U, V and/or W, may also represent CR a and, in the case of X, may also represent CR b , R a representing halogen and R b representing halogen or alkoxy; A 3 represents NHCO, CH 2 CH 2 , CH=CH, COCH 2 , CH(OH)CH 2 , CH2CH(OH), CH(OH)CH(OH) or OCH 2 ; A 4 represents CH 2 , CO, CH 2 CH=CH, COCH=CH or CH 2 CONH; R 2 represents hydrogen, alkyl, hydroxyalkyl, alkylcarbonyloxyalkyl, carbamoyloxyalkyl, carboxyalkyl or carbamoylalkyl; R 3 and R 4 each independently represent hydrogen, hydroxy or alkylcarbonyloxy; or R 3 and R 4 together represent a bridged dimethylmethylenedioxy chain attached to the carbons bearing R 3 and R 4 ; R 5 represents hydrogen, alkyl or hydroxyalkyl; and the dotted line represents a single bond or, when R 3 and R 4 represent hydrogen, also a double bond; and D represents alkyl, aryl or heteroaryl. An example of such an antibiotic is (E)-2-{(2R,3R,6R)-3-[3-(2,5-difluoro-phenyl)- allylamino]-6-[2-(6-methoxy-[l,5]naphthyridin-4-yl)-ethyl]-tetrahydro-pyran-2-yl}-ethanol.

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